JP6129203B2 - α−アミノボロン酸誘導体、選択性免疫プロテアソーム阻害剤 - Google Patents
α−アミノボロン酸誘導体、選択性免疫プロテアソーム阻害剤 Download PDFInfo
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- JP6129203B2 JP6129203B2 JP2014548061A JP2014548061A JP6129203B2 JP 6129203 B2 JP6129203 B2 JP 6129203B2 JP 2014548061 A JP2014548061 A JP 2014548061A JP 2014548061 A JP2014548061 A JP 2014548061A JP 6129203 B2 JP6129203 B2 JP 6129203B2
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- boronic acid
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- IRDYSTDGVPTYRF-UHFFFAOYSA-N [1-acetamido-2-(4-fluorophenyl)ethyl]boronic acid Chemical compound CC(=O)NC(B(O)O)CC1=CC=C(F)C=C1 IRDYSTDGVPTYRF-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
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- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
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| EP11195107.5 | 2011-12-22 | ||
| PCT/EP2012/076595 WO2013092979A1 (en) | 2011-12-22 | 2012-12-21 | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
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| JP (1) | JP6129203B2 (es) |
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| CN (1) | CN104321060B (es) |
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| SG187757A1 (en) | 2010-08-10 | 2013-03-28 | Rempex Pharmaceuticals Inc | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9012491B2 (en) | 2011-08-31 | 2015-04-21 | Rempex Pharmaceuticals, Inc. | Heterocyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9156858B2 (en) | 2012-05-23 | 2015-10-13 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US10561675B2 (en) | 2012-06-06 | 2020-02-18 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| JP6018319B2 (ja) * | 2012-12-03 | 2016-11-02 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 置換トリアゾールボロン酸化合物 |
| WO2014089365A1 (en) | 2012-12-07 | 2014-06-12 | Venatorx Pharmaceuticals, Inc | Beta-lactamase inhibitors |
| CN104981239B (zh) | 2013-01-04 | 2019-01-04 | 莱姆派克斯制药公司 | 硼酸衍生物及其治疗用途 |
| US9101638B2 (en) | 2013-01-04 | 2015-08-11 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| KR20150103269A (ko) * | 2013-01-04 | 2015-09-09 | 렘펙스 파머수티클스 인코퍼레이티드 | 보론산 유도체 및 그의 치료적 용도 |
| JP6346904B2 (ja) | 2013-01-10 | 2018-06-20 | ベナトルクス ファーマシューティカルズ，インク． | ベータ−ラクタマーゼ阻害剤 |
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| USRE49816E1 (en) | 2014-01-10 | 2024-01-30 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
| LT3140310T (lt) | 2014-05-05 | 2019-11-25 | Rempex Pharmaceuticals Inc | Boronato druskų sintezė ir jų panaudojimas |
| EP3139930A4 (en) | 2014-05-05 | 2018-01-17 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| EP3145936B1 (en) | 2014-05-19 | 2020-09-30 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| PT3154989T (pt) * | 2014-06-11 | 2021-05-18 | Venatorx Pharmaceuticals Inc | Inibidores de beta-lactamase |
| JP6700203B2 (ja) * | 2014-07-01 | 2020-05-27 | レンペックス・ファーマシューティカルズ・インコーポレイテッド | ボロン酸誘導体およびその治療的使用 |
| US11202817B2 (en) | 2014-08-18 | 2021-12-21 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
| AU2015327346B2 (en) | 2014-10-01 | 2019-12-05 | Merck Patent Gmbh | Boronic acid derivatives |
| BR112017006622A2 (pt) * | 2014-10-01 | 2018-07-03 | Merck Patent Gmbh | derivados de ácido borônico |
| RU2017115193A (ru) * | 2014-10-01 | 2018-11-06 | Мерк Патент Гмбх | Производные бороновой кислоты |
| MX2017004043A (es) | 2014-10-01 | 2017-07-04 | Merck Patent Gmbh | Derivados de acido boronico. |
| WO2016081297A1 (en) | 2014-11-18 | 2016-05-26 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US20180051041A1 (en) | 2015-03-17 | 2018-02-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP3347008B1 (en) | 2015-09-11 | 2022-03-09 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| EP3362754B1 (en) | 2015-10-15 | 2021-12-22 | Cornell University | Proteasome inhibitors and uses thereof |
| WO2017100537A1 (en) | 2015-12-10 | 2017-06-15 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| CN107151255A (zh) * | 2016-03-06 | 2017-09-12 | 复旦大学 | 硼酸类化合物及其制备方法和用途 |
| MY196909A (en) | 2016-06-30 | 2023-05-09 | Qpex Biopharma Inc | Boronic acid derivatives and therapeutic uses thereof |
| US11267826B2 (en) | 2017-05-26 | 2022-03-08 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| EP3630782A4 (en) | 2017-05-26 | 2021-03-03 | Venatorx Pharmaceuticals, Inc. | PENICILLIN BINDING PROTEIN INHIBITORS |
| PL3672977T3 (pl) | 2017-08-24 | 2022-09-26 | Merck Patent Gmbh | Pochodne kwasu boronowego |
| WO2019075252A1 (en) | 2017-10-11 | 2019-04-18 | Cornell University | PEPTIDOMIMETIC INHIBITORS OF PROTEASOME |
| EP3694864A4 (en) | 2017-10-11 | 2021-10-13 | Qpex Biopharma, Inc. | BORONIC ACID DERIVATIVES AND THEIR SYNTHESIS |
| CN107556336A (zh) * | 2017-10-16 | 2018-01-09 | 康化（上海）新药研发有限公司 | 一种呋喃‑2‑甲烷基硼酸频哪醇酯的合成方法 |
| PL3710457T3 (pl) | 2017-11-16 | 2023-02-20 | Principia Biopharma Inc. | Inhibitory immunoproteasomu |
| MA50906A (fr) | 2017-11-16 | 2020-09-23 | Principia Biopharma Inc | Inhibiteurs d'immunoprotéasome |
| CN108130370B (zh) * | 2018-01-05 | 2020-11-17 | 武汉惠康达科技有限公司 | Psmb8及其抑制剂在制备治疗脂肪肝及其相关疾病药物中的应用 |
| CN112424209A (zh) | 2018-04-20 | 2021-02-26 | Qpex生物制药有限公司 | 硼酸衍生物及其治疗用途 |
| US20210317145A1 (en) | 2018-07-26 | 2021-10-14 | Merck Patent Gmbh | Boronic Acid Derivatives |
| CN113135944A (zh) * | 2020-01-19 | 2021-07-20 | 首药控股(北京)有限公司 | 硼酸衍生物 |
| CN114075227B (zh) * | 2020-08-19 | 2023-07-04 | 北京嵩润医药科技有限责任公司 | 吡唑硼酸类化合物、包含其的药物组合物及它们的用途 |
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| KR20240090392A (ko) * | 2021-10-14 | 2024-06-21 | 쇼우야오 홀딩스 (베이징) 코., 엘티디. | 보론산 유도체 |
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| IL111175A0 (en) * | 1993-10-07 | 1994-12-29 | Du Pont Merck Pharma | Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them |
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| US7332343B2 (en) | 2004-01-16 | 2008-02-19 | Board Of Regents, The University Of Texas System | Determining enantiomeric excess using indicator-displacement assays |
| RS51983B (en) * | 2004-03-30 | 2012-02-29 | Millennium Pharmaceuticals Inc. | SYNTHESIS OF ORGANOBORIC ACID AND ORGANOBORIC ACID COMPOUNDS |
| AU2007319952B2 (en) | 2006-11-14 | 2012-04-26 | Merck Sharp & Dohme Corp. | Tricyclic heteroaromatic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
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| AU2008321443A1 (en) | 2007-11-13 | 2009-05-22 | Novartis Ag | Beta-lactamase inhibitors |
| AR075090A1 (es) * | 2008-09-29 | 2011-03-09 | Millennium Pharm Inc | Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. |
| JP5933523B2 (ja) * | 2010-03-31 | 2016-06-08 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | １−アミノ−２−シクロプロピルエチルボロン酸の誘導体 |
| US8507494B2 (en) | 2010-04-30 | 2013-08-13 | Merck Sharp & Dohme Corp. | Heterocyclic quinolizine derived M1 receptor positive allosteric modulators |
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Also Published As
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|---|---|
| MX352652B (es) | 2017-12-04 |
| BR112014015363A2 (pt) | 2017-06-13 |
| EA201400735A1 (ru) | 2015-04-30 |
| CN104321060B (zh) | 2018-08-07 |
| CA2860142A1 (en) | 2013-06-27 |
| US9688702B2 (en) | 2017-06-27 |
| HK1206261A1 (en) | 2016-01-08 |
| MX2014007362A (es) | 2014-08-01 |
| SG10201605152SA (en) | 2016-08-30 |
| AU2012356890B2 (en) | 2017-06-08 |
| JP2015502387A (ja) | 2015-01-22 |
| EP2793900A1 (en) | 2014-10-29 |
| SG11201403254QA (en) | 2014-07-30 |
| WO2013092979A1 (en) | 2013-06-27 |
| US20140364396A1 (en) | 2014-12-11 |
| IL233200A (en) | 2017-08-31 |
| CA2860142C (en) | 2020-10-27 |
| BR112014015363A8 (pt) | 2017-06-13 |
| ES2699267T3 (es) | 2019-02-08 |
| CN104321060A (zh) | 2015-01-28 |
| AU2012356890A1 (en) | 2014-08-07 |
| EP2793900B1 (en) | 2018-08-22 |
| KR20140114391A (ko) | 2014-09-26 |
| IL233200A0 (en) | 2014-07-31 |
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